SH-I-048A explained

SH-I-048A (SH-i-048A) is a benzodiazepine derivative related in structure to compounds such as flubromazepam and meclonazepam. SH-I-048A is described as a non subtype selective superagonist at the benzodiazepine site of GABA_A receptors,^[1] with a binding affinity of 0.77 nM at the α₁ subtype, 0.17 nM at α₂, 0.38 nM at α₃ and 0.11 nM at α₅.^[2] It has been used to study the functional differences between the different subtypes of the GABA_A receptor.^{[3] [4]}

See also

• GL-II-73
• QH-II-66
• SH-053-R-CH3-2'F

Notes and References

1. Bryan Roth . Obradović AL, Joksimović S, Poe MM, Ramerstorfer J, Varagic Z, Namjoshi O, Batinić B, Radulović T, Marković B, Roth BL, Sieghart W, Cook JM, Savić MM . Sh-I-048A, an in vitro non-selective super-agonist at the benzodiazepine site of GABAA receptors: the approximated activation of receptor subtypes may explain behavioral effects . Brain Research . 2014 . 1554 . 36–48 . 10.1016/j.brainres.2014.01.036 . 24472579 . 3996760 .
2. Clayton T, Poe MM, Rallapalli S, Biawat P, Savić MM, Rowlett JK, Gallos G, Emala CW, Kaczorowski CC, Stafford DC, Arnold LA, Cook JM . 6 . A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model . International Journal of Medicinal Chemistry . 2015 . 430248 . 2015 . 26682068 . 4657098 . 10.1155/2015/430248 . free .
3. Obradović LA, Joksimović S, Poe MM, Timić T, Cook JM, Savić MM . Delayed Behavioral Effects of SH–I–048A, a Novel Nonselective Positive Modulator of Gabaa Receptors, After Peripheral Nerve Injury in Rats. . Acta Veterinaria . June 2014 . 64 . 2 . 189–99 . 10.2478/acve-2014-0018 . free .
4. Elgarf AA, Siebert DC, Steudle F, Draxler A, Li G, Huang S, Cook JM, Ernst M, Scholze P . 6 . Different Benzodiazepines Bind With Distinct Binding Modes to GABAA Receptors . ACS Chemical Biology . 13 . 8 . 2033–2039 . August 2018 . 29767950 . 6102643 . 10.1021/acschembio.8b00144 .